Comparative Pharmacology
Head-to-head clinical analysis: EMTRICITABINE versus EMTRICITABINE RILPIVIRINE TENOFOVIR ALAFENAMIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EMTRICITABINE versus EMTRICITABINE RILPIVIRINE TENOFOVIR ALAFENAMIDE.
EMTRICITABINE vs EMTRICITABINE; RILPIVIRINE; TENOFOVIR ALAFENAMIDE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Nucleoside reverse transcriptase inhibitor; phosphorylated to emtricitabine triphosphate which competes with endogenous deoxycytidine triphosphate and incorporates into viral DNA causing chain termination.
Emtricitabine is a nucleoside reverse transcriptase inhibitor (NRTI); rilpivirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI); tenofovir alafenamide is an NRTI. Combination inhibits HIV-1 replication by blocking reverse transcriptase.
200 mg orally once daily, typically in combination with other antiretroviral agents.
One tablet (emtricitabine 200 mg, rilpivirine 25 mg, tenofovir alafenamide 25 mg) orally once daily with a meal.
None Documented
None Documented
Clinical Note
moderateEmtricitabine + Ribavirin
"Emtricitabine may increase the hepatotoxic activities of Ribavirin."
Clinical Note
moderateLamivudine + Emtricitabine
"The risk or severity of adverse effects can be increased when Lamivudine is combined with Emtricitabine."
Clinical Note
moderateGanciclovir + Emtricitabine
"The risk or severity of adverse effects can be increased when Ganciclovir is combined with Emtricitabine."
Clinical Note
moderateValganciclovir + Emtricitabine
Terminal elimination half-life is approximately 10 hours (range 8–12 hours) in adults with normal renal function; prolonged to >20 hours in severe renal impairment (CrCl <30 mL/min).
Emtricitabine: 10 h (healthy subjects); 8-9 h (HIV-1 infected, once-daily dosing achieves therapeutic plasma concentrations). Rilpivirine: 45 h (terminal, supports once-daily dosing). Tenofovir alafenamide: 0.51 h (parent); tenofovir metabolite: 32-37 h (intracellular, supports once-daily dosing).
Renal: approximately 86% of the dose is excreted unchanged in urine via glomerular filtration and active tubular secretion. Biliary/fecal: minimal (<14% as unchanged drug and metabolites in feces).
Emtricitabine: 86% renal (glomerular filtration and active tubular secretion), 14% fecal. Rilpivirine: 85% fecal (65% as parent drug), 6.1% renal (negligible unchanged). Tenofovir alafenamide: <1% renal; >80% fecal as metabolites; hydrolyzed intracellularly to tenofovir, which is eliminated renally (70-80% unchanged) via glomerular filtration and active tubular secretion.
Category C
Category A/B
Antiretroviral, NRTI
NRTI
"The risk or severity of adverse effects can be increased when Valganciclovir is combined with Emtricitabine."